Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif

被引：70
|
作者：
Jagerovic, N
Hernandez-Folgado, L
Alkorta, I
Goya, P
Navarro, M
Serrano, A
de Fonseca, FR
Dannert, MT
Alsasua, A
Suardiaz, M
Pascual, D
Martín, MI
机构：
[1] CSIC, Inst Quim Med, E-28006 Madrid, Spain
[2] Univ Complutense Madrid, Dept Psicobiol, Fac Psicol, E-28040 Madrid, Spain
[3] Fdn Hosp Carlos Haya, E-29010 Malaga, Spain
[4] Univ Complutense Madrid, Fac Med, E-28040 Madrid, Spain
[5] Univ Rey Juan Carlos, Unidad Farmacol, Fac Ciencias Salud, E-28922 Madrid, Spain
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 11期
关键词：
D O I：
10.1021/jm031099y
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new series of 1,2,4-triazoles have been prepared and the evaluation of their cannabinoid properties have been carried out. Compound 8 showed cannabinoid silent antagonist activity in mouse vas deferens and guinea pig ileum preparations and in vivo assays (cannabinoid tetrad) in mouse. It did not have intrinsic activity in these bioassays, and therefore, it did not behave as a partial agonist or an inverse agonist.
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收藏
页码：2939 / 2942
页数：4
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